Functional evolution of the pregnane X receptor

M Iyer, EJ Reschly, MD Krasowski - Expert opinion on drug …, 2006 - Taylor & Francis
The pregnane X receptor (PXR; NR1I2) is a nuclear hormone receptor (NR) that
transcriptionally regulates genes encoding transporters and drug-metabolising enzymes in …

The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution

SA Jones, LB Moore, JL Shenk, GB Wisely… - Molecular …, 2000 - academic.oup.com
Transcription of genes encoding cytochrome P450 3A (CYP3A) monooxygenases is
induced by a variety of xenobiotics and natural steroids. There are marked differences in the …

Pregnane X Receptor Represses HNF4α Gene to Induce Insulin-Like Growth Factor–Binding Protein IGFBP1 that Alters Morphology of and Migrates HepG2 Cells

S Kodama, Y Yamazaki, M Negishi - Molecular pharmacology, 2015 - ASPET
Upon treatment with the pregnane X receptor (PXR) activator rifampicin (RIF), human
hepatocellular carcinoma HepG2-derived ShP51 cells that stably express PXR showed …

Regulation of human pregnane X receptor and its target gene cytochrome P450 3A4 by Chinese herbal compounds and a molecular docking study

YH Liu, SL Mo, HC Bi, BF Hu, CG Li, YT Wang… - Xenobiotica, 2011 - Taylor & Francis
The pregnane X receptor (PXR) plays a critical role in the regulation of human cytochrome
P450 3A4 (CYP3A4) gene. In this study, we investigated the effect of an array of compounds …

Clinical applications of small molecule inhibitors of Pregnane X receptor

JL Staudinger - Molecular and cellular endocrinology, 2019 - Elsevier
The canonical effect of Pregnane X Receptor (PXR, NR1I2) agonism includes enhanced
hepatic uptake and a concomitant increase in the first-pass metabolism and efflux of drugs in …

Activating the pregnane X receptor by imperatorin attenuates dextran sulphate sodium‐induced colitis in mice

M Liu, G Zhang, C Zheng, M Song, F Liu… - British journal of …, 2018 - Wiley Online Library
Background and Purpose Activation of the human pregnane X receptor (PXR; NR1I2) has
potential therapeutic uses for inflammatory bowel disease (IBD). Imperatorin (IMP), a …

The pregnane X receptor down‐regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for (“squelching”) SRC‐1 coactivator

L Hyrsova, T Smutny, A Carazo… - British Journal of …, 2016 - Wiley Online Library
Background and Purpose The organic cation transporter 1 (OCT1) transports cationic drugs
into hepatocytes. The high hepatic expression of OCT1 is controlled by the HNF4α and USF …

[HTML][HTML] The F-box-only protein 44 regulates pregnane X receptor protein level by ubiquitination and degradation

RRF Gee, AD Huber, J Wu, R Bajpai… - … Pharmaceutica Sinica B, 2023 - Elsevier
Pregnane X receptor (PXR) is a ligand-activated nuclear receptor that transcriptionally
upregulates drug-metabolizing enzymes [eg, cytochrome P450 3A4 (CYP3A4)] and …

A phosphomimetic mutation at threonine-57 abolishes transactivation activity and alters nuclear localization pattern of human pregnane x receptor

SR Pondugula, C Brimer-Cline, J Wu… - Drug metabolism and …, 2009 - ASPET
The pregnane X receptor (PXR) plays crucial roles in multiple physiological processes.
However, the signaling mechanisms responsible are not well defined; it is most likely that …

Pregnane X receptor: prediction and attenuation of human CYP3A4 enzyme induction and drug–drug interactions

MW Sinz - Annual Reports in Medicinal Chemistry, 2008 - Elsevier
Publisher Summary Drug–drug interactions are estimated to be responsible for 20–30% of
all adverse drug reactions and the risk of significant drug interactions increases with the …